Projects funded by the NCN
Novel, rationally designed modulators of glycosomal import of enzymes in Trypanosoma parasites
2018/31/B/NZ7/02089
Keywords:
medicinal chemistry protein-protein interaction inhibitors PPI glycosome
Descriptors:
- NZ7_14: Pharmacy, pharmacotherapy, pharmacology
- NZ1_10: Microbiology
- NZ6_6: Parasitology
Panel:
NZ7 - Diagnostic tools, therapies and public health: public health, epidemiology, environmental health risks and occupational medicine, medical ethics, drug discovery and therapies, pharmacology
Host institution :
Warszawski Uniwersytet Medyczny, Wydział Farmaceutyczny
woj. mazowieckie
Principal investigator (from the host institution):
Number of co-investigators in the project: 4
Call: OPUS 16 - announced on 2018-09-14
Amount awarded: 1 719 100 PLN
Project start date (Y-m-d): 2019-07-08
Project end date (Y-m-d): 2024-07-07
Project duration:: 36 months (the same as in the proposal)
Project status: Project completed
Project description
Download the project description in a pdf file
Note - project descriptions were prepared by the authors of the applications themselves and placed in the system in an unchanged form.
Information in the final report
- Publication in academic press/journals (4)
- Computer-Aided Design and Synthesis of a New Class of PEX14 Inhibitors: Substituted 2,3,4,5- tetrahydrobenzo[f][1,4]oxazepines as Potential New Trypanocidal AgentsAuthors:Roberto Fino, Dominik Lenhart, Vishal C. Kalel, Charlotte A. Softley, Valeria Napolitano, Ryan Byrne, Wolfgang Schliebs, Maciej Dawidowski, Ralf Erdmann, Michael Sattler, Gisbert Schneider, Oliver Plettenburg, Grzegorz Popowicz*Academic press:Journal of Chemical Information and Modeling (rok: 2021, tom: 61, strony: 5256−5268), Wydawca: American Chemical SocietyStatus:PublishedDOI:10.1021/acs.jcim.1c00472 - link to the publication
- Structure−Activity Relationship in Pyrazolo[4,3‑c]pyridines, First Inhibitors of PEX14−PEX5 Protein−Protein Interaction with Trypanocidal ActivityAuthors:Maciej Dawidowski,* Vishal C. Kalel, Valeria Napolitano, Roberto Fino, Kenji Schorpp, Leonidas Emmanouilidis, Dominik Lenhart, Michael Ostertag, Marcel Kaiser, Marta Kolonko, Bettina Tippler, Wolfgang Schliebs, Grzegorz Dubin, Pascal Mäser, Igor V. Tetko, Kamyar Hadian, Oliver Plettenburg, Ralf Erdmann, Michael Sattler* , Grzegorz M. Popowicz*Academic press:Journal of Medicinal Chemistry (rok: 2020, tom: 63, strony: 847-879), Wydawca: American Chemical SocietyStatus:PublishedDOI:10.1021/acs.jmedchem.9b01876 - link to the publication
- Structure-based design, synthesis and evaluation of a novel family of PEX5-PEX14 interaction inhibitors against TrypanosomaAuthors:Valeria Napolitano,* Piotr Mróz, Monika Marciniak, Vishal C. Kalel, Charlotte A. Softley, Julian D. Janna Olmos, Bettina G. Tippler, Kenji Schorpp, Sarah Rioton, Tony Fröhlich, Oliver Plettenburg, Kamyar Hadian, Ralf Erdmann, Michael Sattler, Grzegorz M. Popowicz, Maciej Dawidowski,* Grzegorz Dubin*Academic press:European Journal of Medicinal Chemistry (rok: 2022, tom: 243, strony: 114778), Wydawca: ElsevierStatus:PublishedDOI:10.1016/j.ejmech.2022.114778 - link to the publication
- Water envelope has a critical impact on the design of protein–protein interaction inhibitorsAuthors:Ekaterina L. Ratkova,* Maciej Dawidowski, Valeria Napolitano, Grzegorz Dubin, Roberto Fino, Michael S. Ostertag, Michael Sattler, Grzegorz Popowicz* Igor V. Tetko*Academic press:Chemical Communications (rok: 2020, tom: 56, strony: 4360-4363), Wydawca: Royal Society of ChemistryStatus:PublishedDOI:10.1039/C9CC07714F - link to the publication